Assay Detail
Binding
CHEMBL841027
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Displacement of [125I]p-iodoclonidine from imidazoline receptor I-1 in rat pheochromocytoma cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.73 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2092861 | — | — | 1 | 8.97 |
| CHEMBL71429 | — | — | 1 | 8.30 |
| CHEMBL94022 | — | — | 1 | 7.93 |
| CHEMBL67706 | — | — | 1 | 7.76 |
| CHEMBL275970 | TRACIZOLINE | — | 1 | 7.72 |
| CHEMBL57895 | EFAROXAN | 2.0 | 1 | 7.14 |
| CHEMBL273485 | — | — | 1 | 6.51 |
| CHEMBL93845 | — | — | 1 | 6.46 |
| CHEMBL1907831 | — | — | 1 | 6.23 |
| CHEMBL14640 | — | — | 1 | 6.15 |
| CHEMBL14210 | PHENYZOLINE | — | 1 | 5.43 |
| CHEMBL68608 | — | — | 1 | 5.22 |
| CHEMBL1907832 | — | — | 1 | 5.20 |
| CHEMBL2092860 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2092861 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL71429 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL94022 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL67706 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL275970 | TRACIZOLINE | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL57895 | EFAROXAN | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL273485 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL93845 | — | Ki | = | 346.74 | nM | 6.46 |
| CHEMBL1907831 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL14640 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL14210 | PHENYZOLINE | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL68608 | — | Ki | = | 6025.6 | nM | 5.22 |
| CHEMBL1907832 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL2092860 | — | Ki | = | 7244.36 | nM | 5.14 |